Compounds > mk 4965
Page last updated: 2024-11-12

mk 4965

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Cross-References

ID SourceID
PubMed CID16045418
CHEMBL ID489586
SCHEMBL ID3151052
MeSH IDM0526628

Synonyms (24)

Synonym
920035-77-4
3-{5-[(6-amino-1h-pyrazolo[3,4-b]pyridin-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile
r8e ,
3DRP
3DRR
3-[5-[(6-amino-1h-pyrazolo[3,4-b]pyridin-3-yl)methoxy]-2-chloro-phenoxy]-5-chloro-benzonitrile
mk-4965
benzonitrile, 3-[5-[(6-amino-1h-pyrazolo[3,4-b]pyridin-3-yl)methoxy]-2-chlorophenoxy]-5-chloro-
DB08460
CHEMBL489586 ,
KXDIHAQCVNNLIB-UHFFFAOYSA-N ,
SCHEMBL3151052
z8856wdk9s ,
benzonitrile, 3-(5-((6-amino-1h-pyrazolo(3,4-b)pyridin-3-yl)methoxy)-2-chlorophenoxy)-5-chloro-
unii-z8856wdk9s
AKOS027338691
bdbm50479470
CS-0003309
Q27097666
3-(5-((6-amino-1h-pyrazolo[3,4-b]pyridin-3-yl)methoxy)-2-chlorophenoxy)-5-chlorobenzonitrile
SB20030
A917041
3-[5-[(6-amino-2h-pyrazolo[3,4-b]pyridin-3-yl)methoxy]-2-chlorophenoxy]-5-chlorobenzonitrile
HY-14361

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Further refinement of key compounds in this series to optimize physical properties and pharmacokinetics has resulted in the identification of 8e (MK-4965), which has high levels of potency against wild-type and key mutant viruses, excellent oral bioavailability and overall pharmacokinetics, and a clean ancillary profile."( Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Felock, PJ; Flynn, JA; Lai, MT; Liang, Y; Liu, M; McGaughey, G; Miller, M; Moyer, G; Munshi, V; Perlow-Poehnelt, R; Prasad, S; Reid, JC; Sanchez, R; Sisko, JT; Torrent, M; Tucker, TJ; Tynebor, RM; Vacca, JP; Wan, BL; Williams, TM; Yan, Y, 2008)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Reverse transcriptase/ribonuclease HHuman immunodeficiency virus 1IC50 (µMol)0.00030.00020.00030.0004AID977608
Chain A, Reverse transcriptase/ribonuclease HHuman immunodeficiency virus 1IC50 (µMol)0.00030.00020.00030.0004AID977608
Chain A, Reverse transcriptase/ribonuclease HHIV-1 M:B_HXB2RIC50 (µMol)0.00030.00020.00030.0004AID977608
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.00520.00011.076810.0000AID391221; AID391222; AID391223; AID557019; AID557043; AID557044; AID689702; AID689703; AID689705
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Ki0.00040.00031.552310.0000AID443510; AID635130; AID635131; AID641455; AID641456
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (207)

Assay IDTitleYearJournalArticle
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557049Antiviral activity against HIV1 clade G harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641538Plasma clearance in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641520Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase G190S mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID635135Antiviral activity against Human immunodeficiency virus expressing RT K103N/Y181C double mutant infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID557047Antiviral activity against HIV1 clade D harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557042Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391226Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443690Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443705Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557073Cytotoxicity against activated human PBMC after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635197Plasma protein binding in human2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID557043Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391537Antiviral activity against HIV1 with reverse transcriptase Y188L mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391550Toxicity in cardiovascular dog model assessed as effect on heart rate2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641458Antiviral activity against Human immunodeficiency virus expressing reverse transcriptase K103N mutant infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443703Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443685Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391536Antiviral activity against HIV1 with reverse transcriptase Y181C mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641524Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase K101E/Y181C/G190A triple mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391542Antiviral activity against HIV1 with reverse transcriptase K101E/G190A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443702Antiviral activity against HIV with reverse transcriptase K103N/G190A double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557034Ratio of EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391222Inhibition of HIV1 RT polymerase K103N mutant by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557055Cytotoxicity against human SupT1 cells after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443683Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557037Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391540Antiviral activity against HIV1 with reverse transcriptase P236L mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391551Toxicity in cardiovascular dog model assessed as effect on blood pressure2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443679Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557045Antiviral activity against HIV1 CRF17_BF harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443691Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443526Half life in Beagle dog at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443512Antiviral activity against wild type HIV H9-3B infected in human MT2 cells assessed as inhibition of viral replication measuring p24 level after 3 days in presence of 10% fetal bovine serum2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443510Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV reverse transcriptase K103N mutant assessed as BrdU incorporation by standard ECL assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391531Antiviral activity against wild type HIV1 in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557071Cytotoxicity against activated human macrophage after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557072Cytotoxicity against stationary-phase human macrophage after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443697Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID641545Half life in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641461Cytotoxicity against human MT4 cells up to 8.3 uM2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557057Cytotoxicity against stationary-phase human PBMC after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641467Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase Y188L mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641464Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase K103N mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443694Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391546Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557050Antiviral activity against HIV1 clade H harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443524Volume of distribution in Beagle dog at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557053Antiviral activity against NRTI-, PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443513Antiviral activity against wild type HIV H9-3B infected in human MT2 cells assessed as inhibition of viral replication measuring p24 level after 3 days in presence of 50% normal human serum2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391520Clearance in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635128Cytotoxicity against human MT4 cells2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391223Inhibition of HIV1 RT polymerase Y181C mutant by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443699Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557040Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443682Antiviral activity against HIV with reverse transcriptase G190S mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391549Toxicity in cardiovascular dog model assessed as effect on QTc intervals2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641463Antiviral activity against wild type Human immunodeficiency virus assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641526Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase L100l/K103N/P225P/H triple mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443698Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391530Solubility at pH 22008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635265Plasma clearance in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391522Volume of distribution in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391541Antiviral activity against HIV1 with reverse transcriptase F227L mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443701Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557033Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N mutant in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557052Antiviral activity against NRTI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391527Volume of distribution in rhesus monkey at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557029Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443686Antiviral activity against HIV with reverse transcriptase Y181C/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391516AUC in Sprague-Dawley rat at 10 mg/kg, po2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635132Antiviral activity against Human immunodeficiency virus expressing wild type RT infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID689702Inhibition of RNA-dependent DNA polymerase activity of wild type N-terminal His6x-tagged HIV 1 reverse transcriptase p66/p51 expressed in Escherichia coli (DE3) rosetta cells preincubated for 30 mins by SPA assay2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID443707Antiviral activity against HIV with reverse transcriptase K103N/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443516Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as inhibition of viral replication measuring p24 level after 3 days in presence of 10% fetal bovine serum2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443522Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391526AUC in rhesus monkey at 10 mg/kg, po2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443688Antiviral activity against HIV with reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID689704Resistant ratio of IC50 for HIV 1 reverse transcriptase K103N mutant to IC50 for wild type HIV 1 reverse transcriptase2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID391538Antiviral activity against HIV1 with reverse transcriptase V106A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635131Inhibition of Human immunodeficiency virus reverse transcriptase Y181C mutant by SPA assay2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID641530Volume of distribution in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557024Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase L100I mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557041Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635196Antiviral activity against Human immunodeficiency virus expressing RT K103N/Y181C double mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID557028Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557067Plasma protein binding in HIV1 infected patient2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443708Antiviral activity against HIV with reverse transcriptase V106A/G190A/F227L mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443684Antiviral activity against HIV with reverse transcriptase K103N/Y181C double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391524Half life in rhesus monkey at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557020Antiviral activity against HIV1 clade B harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557058Cytotoxicity against stationary-phase human monocyte after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641603Dose normalised AUC in Sprague-Dawley rat at 10 mg/kg, po by LC-MS analysis2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID635137Cytotoxicity against human MT4 cells up to 8.3 uM2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID443532Oral bioavailability in rhesus monkey at 1 mg/kg2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443706Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443677Antiviral activity against HIV with reverse transcriptase L100I mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443687Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443517Clearance in Sprague-Dawley rat at 2 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391517Volume of distribution in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443528Clearance in rhesus monkey at 1 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557051Antiviral activity against PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641466Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase L100l mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443696Antiviral activity against HIV with reverse transcriptase Y181C mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID689705Inhibition of RNA-dependent DNA polymerase activity of N-terminal His6x-tagged HIV 1 reverse transcriptase Y181C mutant expressed in Escherichia coli (DE3) rosetta cells preincubated for 30 mins by SPA assay2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID635136Antiviral activity against Human immunodeficiency virus expressing wild type RT infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID689706Resistant ratio of IC50 for HIV 1 reverse transcriptase Y181C mutant to IC50 for wild type HIV 1 reverse transcriptase2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID641607Solubility of the compound in water at pH 22011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557032Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring reverse transcriptase Y181C mutant in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557026Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase V106A, G190A and F227L mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443509Inhibition of RNA-dependent DNA polymerase activity of wild type HIV reverse transcriptase assessed as BrdU incorporation by standard ECL assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391528Oral bioavailability in rhesus monkey at 10 mg/kg2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557060Selectivity ratio of IC50 for HIV1 isolate R8 reverse transcriptase Y181C mutant to IC50 for HIV1 isolate R8 reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443515Antiviral activity against HIV with reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication measuring p24 level after 3 days in presence of 10% fetal bovine serum2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443675Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557025Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and G190A mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557046Antiviral activity against HIV1 clade C harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557070Cytotoxicity against stationary-phase human CD4+ T cells after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635130Inhibition of Human immunodeficiency virus reverse transcriptase K103N mutant by SPA assay2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID641456Inhibition of Human immunodeficiency virus reverse transcriptase Y181C mutant by SPA assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391543Antiviral activity against HIV1 with reverse transcriptase K103N/G190A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443692Antiviral activity against HIV with reverse transcriptase MDRC4 mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557048Antiviral activity against HIV1 clade F1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557044Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557059Selectivity ratio of IC50 for HIV1 isolate R8 reverse transcriptase K103N mutant to IC50 for HIV1 isolate R8 reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391545Antiviral activity against HIV1 with reverse transcriptase K103N/V179E mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641600Bioavailability in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557022Antiviral activity against HIV1 CRF01_AE harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641454Inhibition of Human immunodeficiency virus reverse transcriptase by SPA assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641537Plasma clearance in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443695Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391547Antiviral activity against HIV1 with reverse transcriptase Y181C/G190A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635266Half life in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391514Half life in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391515Clearance in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641455Inhibition of Human immunodeficiency virus reverse transcriptase K103N mutant by SPA assay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391523Oral bioavailability in Beagle dog at 10 mg/kg2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443700Antiviral activity against HIV with reverse transcriptase L100I/K103N double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557019Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443680Antiviral activity against HIV with reverse transcriptase Y188L mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557023Antiviral activity against HIV1 clade A harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641465Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase Y181C mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557039Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391525Clearance in rhesus monkey at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID635134Antiviral activity against Human immunodeficiency virus expressing RT Y181C mutant infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID443689Antiviral activity against HIV with reverse transcriptase K101E/Y181C/G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443520AUC in Sprague-Dawley rat at 10 mg/kg, po2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443676Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557074Cytotoxicity against activated human monocyte after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635129Inhibition of Human immunodeficiency virus wild type reverse transcriptase by SPA assay2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID443511Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV reverse transcriptase Y181C mutant assessed as BrdU incorporation by standard ECL assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID641606Dose normalised AUC in Beagle dog at 10 mg/kg, po by LC-MS analysis2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443678Antiviral activity against HIV with reverse transcriptase K103N mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391227Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 50% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391548Antiviral activity against HIV1 with reverse transcriptase K103N/Y181C/G190A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID557027Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y188L mutant relative to drug-sensitive HIV1 CNDO2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443521Half life in Sprague-Dawley rat at 2 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557036Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635133Antiviral activity against Human immunodeficiency virus expressing RT K103N mutant infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391534Antiviral activity against HIV1 with reverse transcriptase L100I mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391225Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID689703Inhibition of RNA-dependent DNA polymerase activity of N-terminal His6x-tagged HIV 1 reverse transcriptase K103N mutant expressed in Escherichia coli (DE3) rosetta cells preincubated for 30 mins by SPA assay2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID557021Antiviral activity against HIV1 CRF02_AG harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557031Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant in presence of 10% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID443681Antiviral activity against HIV with reverse transcriptase G190A mutant assessed as inhibition of viral replication2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID641525Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase V106A/G190A/F227L triple mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557035Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641531Volume of distribution in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID557069Cytotoxicity against activated human CD4+ T cells after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641462Antiviral activity against multidrug-resistant Human immunodeficiency virus assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID635264Volume of distribution in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391518Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391544Antiviral activity against HIV1 with reverse transcriptase K103N/P225H mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641457Antiviral activity against Human immunodeficiency virus expressing wild type reverse transcriptase infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443693Antiviral activity against HIV with reverse transcriptase CNDO mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443529Volume of distribution in rhesus monkey at 1 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID635195Antiviral activity against Human immunodeficiency virus expressing RT Y181C mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID391521AUC in Beagle dog at 10 mg/kg, po2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443514Antiviral activity against HIV with reverse transcriptase K103N mutant infected in human MT2 cells assessed as inhibition of viral replication measuring p24 level after 3 days in presence of 10% fetal bovine serum2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID443525AUC in Beagle dog at 1 mg/kg, po2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID641521Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641460Antiviral activity against Human immunodeficiency virus expressing wild type reverse transcriptase infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443523Clearance in Beagle dog at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557030Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID641523Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase K103N/Y181C/G190A triple mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391535Antiviral activity against HIV1 with reverse transcriptase K103N mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID391539Antiviral activity against HIV1 with reverse transcriptase V179E mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641459Antiviral activity against Human immunodeficiency virus expressing reverse transcriptase Y181C mutant infected in human MT4 cells by p24 antigen assay in the presence of 10% FBS2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID689698Cytotoxicity against human CEM174 cells assessed as cell viability2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID391532Antiviral activity against HIV1 with reverse transcriptase G190A mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443530AUC in rhesus monkey at 5 mg/kg, po2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID635194Antiviral activity against Human immunodeficiency virus expressing RT K103N mutant infected in human MT4 cells by p24 antigen assay in the presence of 50% normal human serum2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
AID443518Volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557054Cytotoxicity against human MT4 cells after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID391519Half life in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641468Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase G190A mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID641544Half life in Sprague-Dawley rat at 10 mg/kg, po and 3 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391221Inhibition of wild type HIV1 RT polymerase by SPA2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443527Oral bioavailability in Beagle dog at 1 mg/kg2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID391224Antiviral activity against wild type HIV1 infected in human MT4 cells after 72 hrs in presence of 10% fetal bovine serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID641522Antiviral activity against Human immunodeficiency virus harboring reverse transcriptase K101E/G190A double mutant assessed as inhibition of viral replication2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID443531Half life in rhesus monkey at 1 mg/kg, iv2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID641601Bioavailability in Beagle dog at 10 mg/kg, po and 2 mg/kg, iv2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
AID391533Antiviral activity against HIV1 with reverse transcriptase G190S mutant in presence of 40% normal human serum2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
AID443704Antiviral activity against HIV with reverse transcriptase K103N/P225H double mutant assessed as inhibition of viral replication relative to wild type2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
AID557056Cytotoxicity against human HL60 cells after 24 to 72 hrs by alamar blue assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID557038Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (50.00)29.6817
2010's3 (50.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		2.4620cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
lamivudine
[no description available]		2.0510monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.7430acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
etravirine
[no description available]		2.0510aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		2.0510nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
rilpivirine
[no description available]		2.0610aminopyrimidine;
nitrile		EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
uk 453,061
UK 453,061: a reverse transcriptase inhibitor/anti-HIV agent; structure in first source		2.0610aromatic ether
ConditionIndicatedRelationship StrengthStudiesTrials
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.0610